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US 6,207,391 B1Granted
High-throughput screening assays for modulators of STAT4 and STAT6 activity
AssigneeTularik Inc.
InventorsPengguang Wu, Judi McKinney
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Abstract
This invention provides receptor peptides that have a high affinity for STAT4 and STAT6 polypeptides. Also provided are assays that are useful for identifying compounds that modulate the interaction between STAT4 and STAT6 polypeptides and their respective cellular promoters. The assays are amenable to high throughput screening.
Claims22
A method of screening for modulators of STAT6 binding to a STAT6 receptor, the method comprising:
- incubating a reaction mixture comprising a STAT6 polypeptide, a potential binding modulator, and a receptor peptide which comprises an amino acid sequence YX1X2X3 (SEQ ID NO:61), wherein the tyrosine is phosphorylated and:
- X1 is selected from the group consisting of K, V, R, I, M, and a first nonnatural amino acid;
- X2 is selected from the group consisting of P, A and S;
- and
- X3 is selected from the group consisting of W, Y, F, H, L and an aromatic second nonnatural amino acid;
- with the proviso that the peptide does not include the amino acid sequence YKPF (SEQ ID NO:2) or YKAF;
- and
- determining whether the binding of the STAT6 polypeptide to the receptor peptide is increased or decreased in comparison to an assay which lacks the potential binding modulator.
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